Pharmaceutical formulation

Abstract

A pharmaceutical formulation for a PKC modulatory peptide and a transport moiety comprising the aforementioned components and an anti-aggregant.

1 . An aqueous solution comprising,
 0.25 mg/mL to 5.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),   2.0 mg/mL to 50 mg/mL of an anti-aggregant sugar, and   
       water for injection. 
     
     
         2 . The solution of  claim 1 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol, fructose, sucrose and glycerol. 
     
     
         3 . The solution of  claim 1 , wherein the conjugate is KAI-9803. 
     
     
         4 . The solution of  claim 3 , wherein the anti-aggregant sugar is mannitol. 
     
     
         5 . An aqueous solution comprising,
 0.1 mg/mL to 10 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),   5.0 mg/mL to 40 mg/mL of an anti-aggregant sugar, and   water for injection.   
     
     
         6 . The solution of  claim 5 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol, fructose, sucrose and glycerol. 
     
     
         7 . The solution of  claim 5 , wherein the conjugate is KAI-9803. 
     
     
         8 . The solution of  claim 7 , wherein the anti-aggregant sugar is mannitol. 
     
     
         9 . An aqueous solution comprising,
 2.0 mg/mL to 3.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),   15 mg/mL to 25 mg/mL of an anti-aggregant sugar, and   water for injection.   
     
     
         10 . The solution of  claim 9 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol, fructose, sucrose and glycerol. 
     
     
         11 . The solution of  claim 9 , wherein the conjugate is KAI-9803. 
     
     
         12 . The solution of  claim 11 , wherein the anti-aggregant sugar is mannitol. 
     
     
         13 . An aqueous solution comprising,
 0.5 mg/mL to 5.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),   10.0 mg/mL to 30.0 mg/mL of an anti-aggregant sugar, and   water for injection.   
     
     
         14 . The solution of  claim 13 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol, fructose, sucrose and glycerol. 
     
     
         15 . The solution of  claim 13 , wherein the conjugate is KAI-9803. 
     
     
         16 . The solution of  claim 15 , wherein the anti-aggregant sugar is mannitol. 
     
     
         17 . An aqueous solution comprising,
 2.0 mg/mL to 3.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),   15.0 mg/mL to 25.0 mg/mL of an anti-aggregant sugar, and   water for injection.   
     
     
         18 . The solution of  claim 17 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol, fructose, sucrose and glycerol. 
     
     
         19 . The solution of  claim 17 , wherein the conjugate is KAI-9803. 
     
     
         20 . The solution of  claim 19 , wherein the anti-aggregant sugar is mannitol.